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. 2012 Feb;18(6):755–767. doi: 10.2174/138161212799277752

Table 2F.

Peptides Influencing Aβ Aggregation and Toxicity. Peptides Selected Using Combinatorial Libraries

Name Sequence Description D/L Results Reference

DP1 – DP8 6 residues from:
Ala, Ile, Val, Ser, Thr, Gly
“Decoy” peptides of combinatorial library D Eliminate calcium effect of Aβ1-42 Blanchard et al., 97, 2000 [106, 107]

None Several with 4 groups of consensus sequences: Out of combinatorial library L Inhibit Aβ aggregation Schwarzman et al., 2005 [108]
++H+(H/+)
or
++XX+
or
(D/E)LVH
or
+LVLF

None 12 mers Phage Display with two libraries. L Ligands bind targets in different aggregation states, partly affect aggregation Orner et al., 2006 [109]
Parent molecule: KLVFFKKKKKK
Target: Monomeric and fibrillar Aβ.

ANA1 6 or 15 mers Novel selection involving phage display and counterselection against rat Aβ L Inhibit Aβ toxicity Taddei et al., 2008 [110]
ANA2 e.g. TNPNRRNRTPQMLKR (ANA1)
ANA3

1A, 1B, 2 MSNKGASIGLMAGDVDIADSHA or Combinatorial library and selection based on enzyme EGFP L Inhibitory effect on Aβ aggregation, de-fibrillization Bain et al., 2009 [111]
MSNKGASNALMAGDGDIADSHS or
MQKLDVVAEDAGSNK

D3 RPRTRLHTHRNR Mirror image phage display D Modulates Aβ oligomerization, effective in tg mouse model after oral application Van Groen et al., 2008; Funke et al., 2010 [112, 113]

JM169 Trimer-TEG-D3 Hybrid compound D3 and nonpeptidic β-sheet breaker D In vitro more effective than trimer or D3 Müller-Schiffmann et al., 2010 [115]

1-8 e.g. RAPMGGR or Panning of heptapeptide library against soluble Aβ1-42 L Suppress Aβ1-42 37/48 kDa oligomer formation, keep monomer stable Kawasaki et al., 2010 [128]
RRPVVGR

GN-peptide GNLLTLD Peptide homologous to sequence from apo A-I, selected by phage display L Modulates aggregation, prevents hippocampal neuronal cultures from Aβ induced degeneration Paula-Lima et al., 2009 [119]

D-4F Ac-DWFKAFYDKVAEKFKEAF-NH2 Apo A-I mimetic peptide D Inhibits Aβ deposition and improver cognitive performance of AD tg mice after oral application [120]

D/L: describes peptide conformation. TEG: triethyleneglycol. +: positively charged amino acids. H: hydrophobic amino acid. X: hydrophobic or polar amino acid